title: Effect of lamotrigine on Na(v)1.4 voltage-gated sodium channels.
abstract: Lamotrigine (LTG) is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorder and it has been known that LTG targets voltage-dependent sodium channels (VGSCs). In this study, we investigated the effect of LTG on the Nav1.4 Na(+) current using HEK293 cells expressing mouse Nav1.4 VGSCs. By the treatment of LTG, Nav1.4 Na(+) current was inhibited in a dose-dependent manner. Moreover, 100 μM LTG decreased Nav1.4 Na(+) current around 40% and shifted the V1/2 of the inactivation curve to the hyperpolarization side by 20.96 mV. These findings suggest that LTG inhibits Nav1.4 Na(+) current and modifies the kinetics of the inactivated state.
authors.affiliation: Department of Pharmacotherapeutics, School of Pharmacy, International University of Health and Welfare, Japan.
authors.forename: Yoshihiko
authors.initials: Y
authors.lastname: Nakatani
authors.forename: Haruka
authors.initials: H
authors.lastname: Masuko
authors.forename: Taku
authors.initials: T
authors.lastname: Amano
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D057809:HEK293 Cells; D006801:Humans; D000077213:Lamotrigine; D008564:Membrane Potentials / Q000187:drug effects; D051379:Mice; D018408:Patch-Clamp Techniques; D014227:Triazines / Q000494:pharmacology*; D061567:Voltage-Gated Sodium Channel Blockers / Q000494:pharmacology*; D061566:Voltage-Gated Sodium Channels / Q000187:drug effects*
chemical_list: D000927:Anticonvulsants; D014227:Triazines; D061567:Voltage-Gated Sodium Channel Blockers; D061566:Voltage-Gated Sodium Channels; D000077213:Lamotrigine